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Novel compounds

a technology of cyclopentane and compounds, applied in the field of new substituted cyclopentane compounds, can solve the problems of high morbidity, affecting angioplasty, and substantial quantities of thrombin are unlikely to be presen

Inactive Publication Date: 2005-06-30
ASTRAZENECA AB
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the process of platelet adhesion to the sub-endothelial surface may have an important role to play in the repair of damaged vessel walls, the platelet aggregation that this initiates can precipitate acute thrombotic occlusion of vital vascular beds, leading to events with high morbidity such as myocardial infarction and unstable angina.
The success of interventions used to prevent or alleviate these conditions, such as thrombolysis and platelet-mediated occlusion or re-occlusion also compromises angioplasty.
However, this efficacy may also explain the bleeding problems that have been observed with this class of agent.
Thrombin can produce platelet aggregation largely independently of other pathways but substantial quantities of thrombin are unlikely to be present without prior activation of platelets by other mechanisms.
Thrombin inhibitors such as hirudin are highly effective anti-thrombotic agents, but again may produce excessive bleeding because they function as both anti-platelet and anti-coagulant agents.

Method used

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Examples

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example 1

(4S,5R,6S,7R)-7-[7-[[(1R,2S)-2-Phenylcyclopropyl]amino]-5-(propylthio)-3H-[1,2,3]triazolo[4,5-d]pyrimidin-3-yl]spiro[2.4]heptane-4,5,6-triol

a) (4R / S,7S / R)-Spiro[2.4]hept-5-ene-4,7diol Diacetate

[0044] To a two phase mixture of palladium acetate (1.7 g), lithium acetate dihydrate (123.6 g), lithium chloride (30.0 g), manganese (IV) oxide (15.3 g) and p-benzoquinone (1.4 g) in acetic acid (250 ml), water (420 ml) and pentane (3.7 l) was added spiro[2.4]hepta-4,6-diene (7.7 g) and the resulting mixture was stirred at ambient temperature for 24 hours. The reaction mixture was filtered through a celite plug washing with pentane (1 l). The organic phase was collected, washed successively with saturated sodium bicarbonate solution (500 ml), water (500 ml) and brine (100 ml) then concentrated to dryness under reduced pressure. The residue was absorbed onto silica and purified by chromatography (SiO2; 9:1 isohexane:ethyl acetate) to afford the subtitle compound (2.1 g).

[0045] NMR δH (CDCl3...

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Abstract

The invention provides novel substituted cyclopentane compounds, their use as medicaments, compositions containing them and processes for their preparation.

Description

RELATED APPLICATIONS [0001] This application is a divisional of U.S. application Ser. No. 10 / 399,748, filed on Apr. 21, 2003, which is a national stage filing under 35 U.S.C. 371 of International Application No. PCT / SE01 / 02472, filed Nov. 7, 2001, which claims priority from Sweden Patent Application No. 0004098-0, filed Nov. 9, 2000, the specifications of each of which are incorporated by reference herein. International Application No. PCT / SE01 / 02472 was published under PCT Article 21(2) in English.FIELD OF THE INVENTION [0002] The present invention provides novel substituted cyclopentane compounds, their use as medicaments, compositions containing them and processes for their preparation. BACKGROUND OF THE INVENTION [0003] Platelet adhesion and aggregation are initiating events in arterial thrombosis. Although the process of platelet adhesion to the sub-endothelial surface may have an important role to play in the repair of damaged vessel walls, the platelet aggregation that this i...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/519A61P7/02A61P9/00A61P9/10C07D487/04
CPCC07D487/04A61K31/519A61P7/02A61P9/00A61P9/10
Inventor GUILE, SIMONMARTIN, BARRIE
Owner ASTRAZENECA AB